Abstract:

Breast cancer is the most common invasive cancer among women and a main cause of human death. Chemotherapy
drugs play a key role in breast cancer treatment. The current main problems in chemotherapy are drug toxicity and
drug resistance. The discovery of antitumor drugs suitable for breast cancer therapy remains one of principal challenges.
In our recent anticancer drug discovery screen, 1,2-di(quinazolin-4-yl)diselane (LG003) was found to possess wide spectrum
anticancer efficacy. In the present work, the in vitro anticancer activity of LG003 was evaluated in metastatic breast
cancer cell line MDA-MB-435. Compared with commercial anticancer drug Gefitinib, Oxaliplatin, Epirubicin Hydrochloride,
10-Hydroxycamptothecin and Taxol, LG003 exhibited better or similar antitumor activity which suggests that
LG003 may be a potential anticancer agent for breast cancer. Further treatment time and dose tests indicated LG003 inhibited
MDA-MB-435 cells in time- and dose-dependent way. Direct morphological observation showed that LG003 treatment
resulted in the decrease in cell population size, then apoptosis like shrinking and blebbing, cell membrane damage
and crumbling in turn in a time- and dose-dependent manner. Lactate Dehydrogenase release assay revealed that LG003
executed such effect in MDA-MB-435 cells partly through cytotoxicity which suggests that title compound LG003 can be
used as lead compound for the design and synthesis of more active and low toxicity anticancer drugs for breast cancer
treatment.

Abstract:Breast cancer is the most common invasive cancer among women and a main cause of human death. Chemotherapy
drugs play a key role in breast cancer treatment. The current main problems in chemotherapy are drug toxicity and
drug resistance. The discovery of antitumor drugs suitable for breast cancer therapy remains one of principal challenges.
In our recent anticancer drug discovery screen, 1,2-di(quinazolin-4-yl)diselane (LG003) was found to possess wide spectrum
anticancer efficacy. In the present work, the in vitro anticancer activity of LG003 was evaluated in metastatic breast
cancer cell line MDA-MB-435. Compared with commercial anticancer drug Gefitinib, Oxaliplatin, Epirubicin Hydrochloride,
10-Hydroxycamptothecin and Taxol, LG003 exhibited better or similar antitumor activity which suggests that
LG003 may be a potential anticancer agent for breast cancer. Further treatment time and dose tests indicated LG003 inhibited
MDA-MB-435 cells in time- and dose-dependent way. Direct morphological observation showed that LG003 treatment
resulted in the decrease in cell population size, then apoptosis like shrinking and blebbing, cell membrane damage
and crumbling in turn in a time- and dose-dependent manner. Lactate Dehydrogenase release assay revealed that LG003
executed such effect in MDA-MB-435 cells partly through cytotoxicity which suggests that title compound LG003 can be
used as lead compound for the design and synthesis of more active and low toxicity anticancer drugs for breast cancer
treatment.